Enhancing drug efficacy and therapeutic index through cheminformatics-based selection of small molecule binary weapons that improve transporter-mediated …

JM Grixti, S O'Hagan, PJ Day, DB Kell - Frontiers in Pharmacology, 2017 - frontiersin.org
The transport of drug molecules is mainly determined by the distribution of influx and efflux
transporters for which they are substrates. To enable tissue targeting, we sought to develop …

Pyridonepezils, new dual AChE inhibitors as potential drugs for the treatment of Alzheimer's disease: Synthesis, biological assessment, and molecular modeling

A Samadi, M Estrada, C Pérez… - European journal of …, 2012 - Elsevier
The synthesis, biological assessment and molecular modeling of new pyridonepezils1–8,
able to inhibit human acetylcholinesterase (hAChE) and human butyrylcholinesterase …

[PDF][PDF] The importance of heterocyclic compounds in anti-cancer drug design

S Pearce - Drug Discovery, 2017 - ddw-online.com
Heterocycles are key structural components of many of the anti-cancer drugs available on
the market today. Indeed, of the novel molecular anti-cancer agents approved by the FDA …

Pyrazoline derivatives as promising MAO-A targeting antidepressants: an update

D Choudhary, R Kaur, TG Singh… - Current Topics in …, 2024 - ingentaconnect.com
Depression is one of the key conditions addressed by the Mental Health Gap Action
Programme (mhGAP) of WHO that can lead to self-harm and suicide. Depression is …

Microtubule-Stabilizing 1,2,4-Triazolo[1,5-a]pyrimidines as Candidate Therapeutics for Neurodegenerative Disease: Matched Molecular Pair Analyses and …

T Alle, C Varricchio, Y Yao, B Lucero… - Journal of Medicinal …, 2022 - ACS Publications
Microtubule (MT)-stabilizing 1, 2, 4-triazolo [1, 5-a] pyrimidines (TPDs) hold promise as
candidate therapeutics for Alzheimer's disease (AD) and other neurodegenerative …

Direct and sequential bioactivation of pemigatinib to reactive iminium ion intermediates culminates in mechanism-based inactivation of cytochrome P450 3A

LWT Tang, W Wei, RK Verma, SK Koh, L Zhou… - Drug Metabolism and …, 2022 - ASPET
We recently established the mechanism-based inactivation (MBI) of cytochrome P450 3A
(CYP3A) by the fibroblast growth factor receptor (FGFR) inhibitors erdafitinib and infigratinib …

Therapeutic potential of quinazoline derivatives for Alzheimer's disease: A comprehensive review

Z Haghighijoo, L Zamani, F Moosavi… - European journal of …, 2022 - Elsevier
Quinazolines are considered as a promising class of bioactive heterocyclic compounds with
broad properties. Particularly, the quinazoline scaffold has an impressive role in the design …

Therapeutic Potential of Natural Metabolites Coupled Pyrazole and Its Bio‐Isosteres: Medicinal Perspectives and SAR Studies

B Nehra, M Kumar, PA Chawla, V Chawla - ChemistrySelect, 2024 - Wiley Online Library
Natural products have been extensively explored for their role in drug design and
development to eradicate numerous types of diseases. Also, heterocycles‐based motifs are …

Pyridine ring as an important scaffold in anticancer drugs

A Elagamy, LK Elghoneimy, RK Arafa - … in the synthesis and applications of …, 2023 - Elsevier
Pyridine is a chemical scaffold with growing biological importance. Pyridine-based
compounds represent a useful class of heterocycles found in various chemotherapeutic …

Recent developments in the design and synthesis of benzylpyridinium salts: Mimicking donepezil hydrochloride in the treatment of Alzheimer's disease

S Sepehri, M Saeedi, B Larijani, M Mahdavi - Frontiers in Chemistry, 2022 - frontiersin.org
Background: Alzheimer's disease (AD) is an advanced and irreversible degenerative
disease of the brain, recognized as the key reason for dementia among elderly people. The …